US2013330409A1PendingUtilityA1

Dosage Form

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Assignee: MOHAMMAD HASSANPriority: Dec 9, 2010Filed: Dec 9, 2011Published: Dec 12, 2013
Est. expiryDec 9, 2030(~4.4 yrs left)· nominal 20-yr term from priority
Inventors:Hassan Mohammad
A61P 25/04A61K 31/485A61K 9/2077A61K 9/00A61J 3/00A61K 9/2095A61K 9/2054A61K 45/00A61K 9/5084B29B 9/12A61K 9/1652A61K 31/00A61K 9/205A61K 9/1635A61K 9/2031A61P 25/00A61K 9/1682A61K 9/2027A61K 9/16A61K 9/20
38
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Claims

Abstract

The present invention provides a dosage form, particularly a tamper resistant dosage form, comprising; non-stretched melt extruded particulates comprising a drug selected from an opioid agonist, a tranquilizer, a CNS depressant, a CNS stimulant or a sedative hypnotic; and a matrix; wherein said melt extruded particulates are present as a discontinuous phase in said matrix.

Claims

exact text as granted — not AI-modified
1 . A dosage form comprising:
 non-stretched, melt-extruded particulates comprising a drug selected from an opioid agonist, a tranquilizer, a CNS depressant, a CNS stimulant or a sedative hypnotic; and a matrix;   wherein said melt-extruded particulates are present as a discontinuous phase in said matrix.   
     
     
         2 . The dosage form as claimed in  claim 1 , wherein said drug is an opioid agonist. 
     
     
         3 . The dosage form as claimed in  claim 2 , wherein said opioid agonist is selected from the group consisting of oxycodone, oxymorphone, hydrocodone, hydromorphone, morphine, codeine, buprenorphine, fentanyl, tramadol, and tapentadol, or a pharmaceutically acceptable salt thereof. 
     
     
         4 . The dosage form as claimed in  claim 1 , which comprises 15-80% wt of said melt-extruded particulates, based on the total weight of the dosage form. 
     
     
         5 . The dosage form as claimed in  claim 1 , which comprises 20-85% wt of said matrix, based on the total weight of the dosage form. 
     
     
         6 . The dosage form as claimed in  claim 1 , wherein said matrix comprises a continuous phase comprising a gel-forming agent. 
     
     
         7 . The dosage form as claimed in  claim 1  in the form of a tablet. 
     
     
         8 - 10 . (canceled) 
     
     
         11 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates are microparticulates. 
     
     
         12 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates have a diameter and/or length of less than about 900 μm. 
     
     
         13 . (canceled) 
     
     
         14 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates comprise 3 to 50% wt of drug, based on the total weight of a particulate. 
     
     
         15 . (canceled) 
     
     
         16 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates further comprise a polymer conferring crush resistance. 
     
     
         17 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates further comprise a polymer selected from an acrylic polymer, a methacrylic polymer or a mixture thereof. 
     
     
         18 . The dosage form as claimed in  claim 17 , wherein said polymer is selected from the group consisting of an acrylic acid and methacrylic acid copolymer, a methyl methacrylate copolymer, ethoxyethyl methacrylate, cyanoethyl methacrylate, poly(acrylic acid), poly(methacrylic acid), a methacrylic acid alkylamide copolymer, poly(methyl methacrylate), polymethacrylate, a poly(methyl methacrylate) copolymer, polyacrylamide, a aminoalkyl methacrylate copolymer, poly(methacrylic acid anhydride), and a glycidyl methacrylate copolymer. 
     
     
         19 . The dosage form as claimed in  claim 18 , wherein said acrylic acid and methacrylic acid copolymer is selected from acrylic acid alkyl esters, methacrylic acid alkyl esters and mixtures thereof. 
     
     
         20 . (canceled) 
     
     
         21 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates further comprise a rate controlling or modifying agent. 
     
     
         22 . The dosage form as claimed in  claim 21 , wherein said rate controlling or modifying agent is an alkyl cellulose. 
     
     
         23 . (canceled) 
     
     
         24 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates further comprise a lubricant. 
     
     
         25 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates further comprise a plasticiser. 
     
     
         26 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates comprise oxycodone or hydromorphone, or a hydrochloride salt thereof, an ethyl acrylate and methyl methacrylate copolymer, ethyl cellulose as a rate controlling or modifying agent, stearyl alcohol and/or triethyl citrate as a plasticiser, glyceryl dibehenate as a lubricant and optionally an opioid antagonist. 
     
     
         27 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates comprise an opioid agonist and further comprise an opioid antagonist. 
     
     
         28 . The dosage form as claimed in  claim 1 , wherein said melt-extruded particulates are spherical or near spherical. 
     
     
         29 . The dosage form as claimed in  claim 1 , wherein said matrix comprises a silicone and/or a gel-forming agent. 
     
     
         30 . The dosage form as claimed in  claim 29 , wherein said gel-forming agent is selected from polyethylene oxide, polyvinyl alcohol, hydroxypropyl methyl cellulose, carbomers, poly(uronic) acids or mixtures thereof. 
     
     
         31 . The dosage form as claimed in  claim 29 , wherein said silicone or gel-forming agent is curable. 
     
     
         32 . (canceled) 
     
     
         33 . A process for preparing a dosage form comprising a drug selected from an opioid agonist, a tranquilizer, a CNS depressant, a CNS stimulant or a sedative hypnotic comprising:
 i) melt extruding a composition comprising the drug through extrusion die head orifices of less than 1.0 mm in diameter to form a melt extrudate having an average diameter of less than about 1000 μm;   ii) cutting the melt extrudate to form particulates having an average diameter of less than about 1000 μm;   iii) mixing said particulates with a matrix material so that said particulates form a discontinuous phase in said matrix; and   iv) forming said mixture into a dosage form.   
     
     
         34 . The process as claimed in  claim 33 , further comprising a step of stretching said melt extrudate to form a stretched melt extrudate prior to cutting. 
     
     
         35 . The process as claimed in  claim 33 , wherein in said cutting step a cutter cuts the melt extrudate as it emerges under pressure and still softened from the orifices of the die plate. 
     
     
         36 - 37 . (canceled) 
     
     
         38 . The process as claimed in  claim 33 , wherein said particulates are melt extruded at a temperature of 100° C. or less. 
     
     
         39 . The process as claimed in  claim 33 , comprising a further step of curing said matrix. 
     
     
         40 - 51 . (canceled) 
     
     
         52 . A method of treating a subject in need of pain relief, comprising administering to said subject a dosage form as claimed in  claim 1 . 
     
     
         53 . The dosage form as claimed in  claim 26 , wherein said melt-extruded particulates comprise oxycodone hydrochloride salt or hydromorphone hydrochloride salt. 
     
     
         54 . The dosage form as claimed in  claim 26 , wherein said ethyl acrylate and methyl methacrylate copolymer is Eudragit NE 30 D or NE 40 D. 
     
     
         55 . The dosage form as claimed in  claim 27 , wherein said opioid antagonist is naloxone.

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